Inhibitors of phosphoinositide-3-kinase: a structure-based approach to understanding potency and selectivity

Teather J Sundstrom; Amy C Anderson; Dennis L Wright

doi:10.1039/b819067b

Inhibitors of phosphoinositide-3-kinase: a structure-based approach to understanding potency and selectivity

Org Biomol Chem. 2009 Mar 7;7(5):840-50. doi: 10.1039/b819067b. Epub 2009 Jan 8.

Authors

Teather J Sundstrom¹, Amy C Anderson, Dennis L Wright

Affiliation

¹ Department of Pharmaceutical Sciences, University of Connecticut, 69 N Eagleville Rd, U-3092, Storrs, CT 06269, USA.

PMID: 19225663
DOI: 10.1039/b819067b

Abstract

Phosphoinositide-3-kinase is a pivotal protein involved in a wide variety of signaling cascades and there has been a great deal of interest in the development of potent and selective inhibitors of this enzyme. In this review, the potency and selectivity of the known inhibitors is presented along with key structural information that helps rationalize the observed trends.

Publication types

Research Support, Non-U.S. Gov't
Review

MeSH terms

1-Phosphatidylinositol 4-Kinase / antagonists & inhibitors*
Binding Sites
Protein Binding
Protein Kinase Inhibitors / chemistry*
Protein Kinase Inhibitors / pharmacology
Structure-Activity Relationship

Substances

Protein Kinase Inhibitors
1-Phosphatidylinositol 4-Kinase